Assay Detail
Binding
CHEMBL4730611
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Inhibition of F-Bak (GQVGRQLAIIGDK(6-FAM)INR-amide probe binding to BCL-xl (unknown origin) incubated for 1 hr by TR-FRET assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 8.76 | 10.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3935328 | — | — | 1 | 10.57 |
| CHEMBL3891330 | — | — | 1 | 10.36 |
| CHEMBL3972984 | — | — | 1 | 9.53 |
| CHEMBL3901568 | — | — | 1 | 9.48 |
| CHEMBL3912857 | — | — | 1 | 9.19 |
| CHEMBL3910958 | — | — | 1 | 8.30 |
| CHEMBL3983880 | — | — | 1 | 8.22 |
| CHEMBL3287296 | — | — | 1 | 7.96 |
| CHEMBL3287293 | — | — | 1 | 7.19 |
| CHEMBL3287292 | — | — | 1 | 6.79 |
| CHEMBL3919588 | — | — | 1 | - |
| CHEMBL3793424 | — | — | 1 | - |
| CHEMBL4762875 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3935328 | — | Ki | = | 0.027 | nM | 10.57 |
| CHEMBL3891330 | — | Ki | = | 0.044 | nM | 10.36 |
| CHEMBL3972984 | — | Ki | = | 0.296 | nM | 9.53 |
| CHEMBL3901568 | — | Ki | = | 0.329 | nM | 9.48 |
| CHEMBL3912857 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL3910958 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3983880 | — | Ki | = | 5.96 | nM | 8.22 |
| CHEMBL3287296 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL3287293 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL3287292 | — | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL3919588 | — | Ki | = | 0.008 | nM | - |
| CHEMBL3793424 | — | Ki | < | 0.01 | nM | - |
| CHEMBL4762875 | — | Ki | < | 0.01 | nM | - |